TP-024

Agonist of GPR52

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe TP-024 is in the process of SERP review.

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Information

GPR52

Agonist

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Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Cell:

No significant activity at 10 μM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

TP-024 (also called FTBMT) is a well-characterized potent GPR52 agonist (orphan receptor). It show good selectivity in several selectivity panels (including receptors, ion channels & enzymes). TP-024 has similar activity against human, mouse and rat GPR52. In CHO cells (overexpressing GPR52) it dose-dependently stimulated cAMP production and modulation of the corresponding downstream effects. Good pharmacokinetic properties allow the use in mouse and rat animal models. HTL0041178 could be an additional orthogonal probe for the GPR52 receptor to be included in your in vitro studies.

(last updated: 7 Apr 2025 )

SERP+ Ratings

In Cell Rating

In Model Organisms

SERP+ Comments:

GPR52 agonists PW0787 and HTL0041178 both have comparable potency, selectivity and more in vivo PK characterisation.

(last updated: 14 Oct 2025 )